Smoothened Receptors

Smoothened (Smo) receptors are non-classical G-protein-coupled receptors that belong to the Frizzled family. Smoothened receptors lack the ability to directly interact with their endogenous ligand, Hedgehog (Hh). In the resting state, Smo receptors are bound to patched (Ptc).

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
4918 GSA 10
Smo receptor agonist
4551 Purmorphamine
Smo receptor agonist
4366 SAG
Potent Smoothened receptor agonist; activates the Hedgehog signaling pathway

Antagonists

Cat No Product Name / Activity
1623 Cyclopamine
Inhibitor of Hedgehog (Hh) signaling; Smo antagonist
5554 IHR 1
Potent Smo antagonist
5561 IHR-Cy3
Potent fluorescent Smo antagonist
5981 Itraconazole
SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623)
4717 Jervine
Inhibitor of Hedgehog (Hh) signaling; binds directly to Smo
4917 M 25
Potent Smoothened (Smo) receptor antagonist
4585 MRT 10
Smoothened (Smo) antagonist
5262 PF 5274857 hydrochloride
High affinity and selective Smoothened (Smo) receptor antagonist
1974 SANT-1
Inhibitor of Hedgehog (Hh) signaling; antagonizes smoothened activity
3617 SANT-2
Inhibitor of Hedgehog (Hh) signaling; antagonizes smoothened activity

Other

Cat No Product Name / Activity
4474 20(S)-Hydroxycholesterol
Allosteric activator of Hedgehog signaling; induces Smo accumulation
4662 SMANT hydrochloride
Inhibits Smoothened (Smo) accumulation

Related Targets

    Smoothened (Smo) receptors are non-classical G-protein-coupled receptors that belong to the Frizzled family. Smoothened receptors lack the ability to directly interact with their endogenous ligand, Hedgehog (Hh). In the resting state, Smo receptors are bound to and repressed by patched (Ptc).

    Upon Hh-Ptc interaction, Smo receptors are liberated and phosphorylated (activated). This initiates a signaling cascade that controls the activity of transcription factors belonging to the Gli family (particularly Cubitus interruptus (Ci)). Smo receptors are vital for embryogenesis (segmentation and appendage development) and are involved in maintenence of tissue homeostasis in adults. The human gene encoding the Smo receptor has been localized on chromosome 7q32.3.

    External sources of pharmacological information for Smoothened Receptors :

      Literature for Smoothened Receptors

      GPCR

      GPCR Product Listing

      A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

      • Rhodopsin-like Receptors
      • Secretin-like Receptors
      • Glutamate Receptors
      • Frizzled Receptors
      • GPCR Signaling

      Smoothened Receptor Gene Data

      Species Gene Symbol Gene Accession No. Protein Accession No.
      Human SMO NM_005631 Q99835
      Mouse Smo NM_176996 P56726
      Rat Smo NM_012807 P97698